YQ128

2454246-18-3

545.11

DMSO : 250 mg/mL (458.62 mM; Need ultrasonic)

Immunology/Inflammation; Immunology/Inflammation

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC₅₀ of 0.30 uM. YQ128 significantly and selectively suppresses the production of IL-1beta, but not TNF-alpha, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity^[1]. In Vitro: YQ128 (0.3-100 uM; 30 mins) dose dependently suppressed the release of IL-1beta from peritoneal macrophages upon LPS/ATP challenge with an IC₅₀ of 1.59 uM^[1].
YQ128 (20 uM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells^[1].
In Vivo: YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration^[1].
YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a t_max and c_max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F_oral) is estimated as 10%^[1].
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd_ss) of 8.5 L/kg and rapid total clearance (CL_tot) of 41 mL/min/kg^[1].
YQ128 (10 mg/kg) has been shown to trigger IL-1beta production in a NLRP3- dependent manner in C57BL/6 mice^[1].